Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/282)
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Publication number: 20080281100Abstract: The present invention provides pure paliperidone comprising less than about 0.1%, preferably less than about 0.05% and more preferably less than about 0.02%, impurity X as well as purification processes to obtain thereof.Type: ApplicationFiled: February 14, 2008Publication date: November 13, 2008Inventors: Santiago INI, Naama CHASID, Kobi CHEN, Osnat PORTER-KLEKS
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Publication number: 20080262227Abstract: The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel acetic acid salt thereof, which affords, inter alia, resolution of the isomers and/or by heat conversion.Type: ApplicationFiled: June 18, 2008Publication date: October 23, 2008Inventors: Pavel Slanina, Jiri Bartl
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Publication number: 20080249112Abstract: The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The invention also related to pharmaceutical compositions comprising such compounds, methods of treating cancer by the administration of such compositions, and processes for the preparation of the compounds. Compounds of the invention have the following formula: formula (I).Type: ApplicationFiled: April 6, 2005Publication date: October 9, 2008Applicant: CHIRON CORPORATIONInventors: Weibo Wang, Ryan N. Constantine, Liana M. Lagniton
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Publication number: 20080214808Abstract: The present invention concerns a process for preparing aseptic crystalline 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one palmitate ester (I) substantially free of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (II-a), 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3 -yl)-1-piperidinyl]ethyl]-6,7-dihydro-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (II-b), and 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-ethyl]-6,7,8,9-tetrahydro-2-methyl-9-pentadecyl-4H-pyrido[1,2-a]pyrimidin-4-one (III), and having an average particle size ranging from 20 to 150 ?m.Type: ApplicationFiled: April 20, 2006Publication date: September 4, 2008Inventors: Thomas Frederik Ernestine Spittaels, Joannes Petrus Van Dun, Jurgen Alois Verbraeken, Benny Wouters
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Publication number: 20080214809Abstract: The present invention provides processes of preparing 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate.Type: ApplicationFiled: February 27, 2008Publication date: September 4, 2008Inventors: Ben-Zion Dolitzky, Evgeny Shapiro, Santiago Ini, Yaron Shmuely, Eli Lancry, Gideon Pilarsky
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Patent number: 7420056Abstract: Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related methods of treatment are also provided.Type: GrantFiled: March 14, 2007Date of Patent: September 2, 2008Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Stefan Oberboersch, Corinna Sundermann, Michael Haurand, Ruth Jostock, Klaus Schiene, Thomas Tzschentke, Thomas Christoph, Dagmar Kaulartz, Saskia Zemolka
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Publication number: 20080200479Abstract: The invention relates to new salts of ocaperidone and uses thereof, particularly in the pharmaceutical industry. The invention discloses specific salts of ocaperidone having increased water solubilities, as well as therapeutic methods by administering said salts, in particular for treating various diseases of the central or peripheral nervous system, especially central nervous system. It further deals with pharmaceutical compositions comprising said salts and methods for preparing the same.Type: ApplicationFiled: February 24, 2006Publication date: August 21, 2008Inventors: Stefano Biondi, Arnold Demailly, Cesare Mondadori, Jean-Laurent Paparin
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Publication number: 20080200676Abstract: The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]- pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.Type: ApplicationFiled: August 23, 2007Publication date: August 21, 2008Inventors: Ben-Zion Dolitzky, Evgeny Shapiro, Santiago Ini, Yaron Shmuely, Eli Lancry
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Patent number: 7414045Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 18, 2003Date of Patent: August 19, 2008Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Patent number: 7405298Abstract: The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel acetic acid salt thereof, which affords, inter alia, resolution of the isomers and/or by heat conversion.Type: GrantFiled: November 13, 2003Date of Patent: July 29, 2008Assignee: Synthon IP Inc.Inventors: Pavel Slanina, Jiri Bartl
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Publication number: 20080177067Abstract: The present invention provides amorphous and crystalline forms of Paliperidone, and processes for preparing thereof.Type: ApplicationFiled: August 14, 2007Publication date: July 24, 2008Inventors: Ben-Zion Dolitzky, Santiago Ini, Naama Chasid, Yaron Shmuely, Kobi Chen, Eli Lancry
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Publication number: 20080176860Abstract: The present invention relates to compounds of the formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: January 21, 2008Publication date: July 24, 2008Inventor: Lutz Weber
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Publication number: 20080176869Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: March 12, 2008Publication date: July 24, 2008Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Publication number: 20080171875Abstract: The present invention relates to a process for preparing paliperidone from its intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one.Type: ApplicationFiled: August 14, 2007Publication date: July 17, 2008Inventors: Santiago Ini, Naama Chasid, Yaron Shmuely, Kobi Chen
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Publication number: 20080171876Abstract: The present invention provides pure paliperidone as well as purification processes to obtain thereof.Type: ApplicationFiled: August 14, 2007Publication date: July 17, 2008Inventors: Santiago Ini, Naama Chasid, Kobi Chen, Osnat Porter-Kleks
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Patent number: 7326711Abstract: Pyridin[1,2-a]pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: GrantFiled: June 17, 2004Date of Patent: February 5, 2008Assignee: Chiron CorporationInventors: Weibo Wang, Ryan N. Constantine, Liana Marie Lagniton, Sabina Pecchi, Matthew T. Burger, Manoj C. Desai
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Patent number: 7320980Abstract: The invention relates to substituted pyrido[1,2-a]pyrimidine compounds corresponding to formula (I) wherein: R1, R2 and R3 are as defined in the specification. Related pharmaceutical formulations and methods for inhibiting nitrogen oxide synthesis (NOS) and other treatments are also provided.Type: GrantFiled: September 6, 2005Date of Patent: January 22, 2008Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Helmut Buschmann, Ullvi Bluhm, Bernd Clement, Dieter Heber, Ulrich Wolschendorf
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Publication number: 20080004265Abstract: The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: ApplicationFiled: June 26, 2007Publication date: January 3, 2008Inventors: Michael A. Walker, Chen Li, Katharine A. Grant-Young, John D. Matiskella, B. Narasimhulu Naidu, Jacques Banville, Francis Beaulieu, Carl Ouellet, Annapurna Pendri, Roger Remillard, Yasutsugu Ueda, Ting T. Yin
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Patent number: 7307168Abstract: The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent.Type: GrantFiled: November 13, 2002Date of Patent: December 11, 2007Assignee: EGIS Gyógyszergyár Rt.Inventors: László Pongó, József Reiter, Gyula Simig, Gábor Berecz, György Clementis, Péter Slégel, János Szulágyi, László Koncz, Györgyi Vereczkeyné Donáth, Kálmán Nagy, Gyuláné Körtvélyessy
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Patent number: 7271170Abstract: Compounds of Formula I are provided, as are methods for their preparation. The variables Z1, Z2, Z3, R4, R5, R6, R7, R8 and Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAA receptors (e.g., receptor localization studies).Type: GrantFiled: July 23, 2004Date of Patent: September 18, 2007Assignee: Neurogen CorporationInventors: Linghong Xie, Bingsong Han, Yuelian Xu, George Maynard, Bertrand L. Chenard, Kenneth Shaw, Yang Gao
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Patent number: 7256195Abstract: The present invention is directed to the novel forms of risperidone, designated Form A, Form B and Form E. Methods for their preparation are also disclosed. The present invention also relates to processes for making risperidone. Pharmaceutical compositions containing the new forms of risperidone and methods of using them are also disclosed.Type: GrantFiled: September 23, 2003Date of Patent: August 14, 2007Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Barnaba Krochmal, Dov Diller, Ben-Zion Dolitzky, Judith Aronhime
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Patent number: 7230103Abstract: Substituted 3,4-dihydropyrido[1,2-a]pyrimidines of formula I and processes for the production thereof Also disclosed are substance libraries and pharmaceutical compositions containing the compound, and methods of treatment for pain, urinary incontinence, pruritus, tinnitus and/or diarrhoea using the pharmaceutical composition.Type: GrantFiled: April 11, 2003Date of Patent: June 12, 2007Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul, Utz-Peter Jagusch
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Patent number: 7211572Abstract: The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.Type: GrantFiled: October 13, 2005Date of Patent: May 1, 2007Assignee: Japan Tobacco Inc.Inventors: Susumu Miyazaki, Susumu Katoh, Kaoru Adachi, Hirotaka Isoshima, Satoru Kobayashi, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Shinichi Kiyonari, Shuichi Wamaki
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Patent number: 7205405Abstract: The process consists in condensing (2-methyl-6,7,8,9-tetrahydro-4 H-pyrido-[1,2-a]pyrimidin-3-yl)-acetaldehyd with 6-fluoro-3-piperidinyl)-1,2-benzisoxazole to yield the intermediate enamine, 3-{2-[4-(6-fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]vinyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2,-a]pyrimidin-4 -one followed by reduction of such an enamine.Type: GrantFiled: March 3, 2003Date of Patent: April 17, 2007Assignee: Ferrer Internacional, S.A.Inventors: Rafael Foguet, Jorge Ramentol, Diego Fernandez-Cano, Miguel P. Armengol, Francesc X. Camps, Juan Sallares, Inés Petschen, Mireia Pasto, Esther Gordo
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Patent number: 7202360Abstract: Risperidone is prepared in a high yield by reacting 2,4-difluorophenyl(4-piperidinyl)methanone oxime hydrochloride and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in an aqueous alkali hydroxide solution having an alkali hydroxide concentration in the range of 20 to 40%.Type: GrantFiled: October 17, 2003Date of Patent: April 10, 2007Assignee: Hanmi Pharm Co., Ltd.Inventors: Nam-Du Kim, Jae-Heon Lee, Moon-Sub Lee, Young-Kil Chang, Gwan-Sun Lee
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Patent number: 7173022Abstract: The invention encompasses a series cyclic bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS.Type: GrantFiled: May 26, 2005Date of Patent: February 6, 2007Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Jacques Banville, John D. Matiskella, Serge Plamondon, Yasutsugu Ueda
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Patent number: 7141564Abstract: Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.Type: GrantFiled: May 24, 2002Date of Patent: November 28, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Gerald Brooks, David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, Neil David Pearson
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Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
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Patent number: 7074929Abstract: This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y.Type: GrantFiled: November 10, 2003Date of Patent: July 11, 2006Assignees: Neurogen Corp., Pfizer, Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 7067662Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory and immune conditions and diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of a chemokine receptor. The subject methods are useful for the treatment of inflammatory and immunoregulatory disorders and diseases, such as multiple sclerosis, rheumatoid arthritis and type I diabetes.Type: GrantFiled: September 21, 2004Date of Patent: June 27, 2006Assignee: Amgen SF, LLCInventors: Julio C. Medina, Michael G. Johnson, An-Rong Li, Jiwen Liu, Alan Xi Huang, Liusheng Zhu, Andrew P. Marcus
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Patent number: 7056917Abstract: A medicament for preventive and/or therapeutic treatment of a microbial infection which comprises as an active ingredient a compound represented by the following general formula (I): wherein, R1 and R2 represent hydrogen atom, a halogen atom, hydroxyl group or the like, W1 represents —CH?CH—, —CH2O—, —CH2CH2— or the like; R3 represents hydrogen atom, a halogen atom, hydroxyl group or an amino group; R4 represents hydrogen atom, a group of —OZ0-4R5 (Z0-4 represents an alkylene group, a fluorine-substituted alkylene group or a single bond, and R5 represents a cyclic alkyl group, an aryl group or the like); W2 represents a single bond or —C(R8)?C(R9)— (R8 and R9 represent hydrogen atom, a halogen atom, a lower alkyl group or the like, Q represents an acidic group, but W2 and Q may together form vinylidenethiazolidinedione or an equivalent heterocyclic ring; m and n represent an integer of 0 to 2, and q represents an integer of 0 to 3.Type: GrantFiled: April 26, 2001Date of Patent: June 6, 2006Assignees: Daiichi Pharmaceutical Co., Ltd., Trine Pharmaceuticals, Inc.Inventors: Kiyoshi Nakayama, Masami Ohtsuka, Haruko Kawato, William Watkins, Jason Zhang, Monica Palme, Aesop Cho
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Patent number: 7030128Abstract: A class of imidazo[1,2-?]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: GrantFiled: March 19, 2002Date of Patent: April 18, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Philip Jones, Richard Thomas Lewis, Angus Murray MacLeod, Robert James Maxey, Kevin William Moore, Leslie Joseph Street
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Patent number: 6933300Abstract: Inhibitors of JAK3 kinase for the treatment of allergy, and others are described.Type: GrantFiled: April 23, 2002Date of Patent: August 23, 2005Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Ravi Malavia, Elise A. Sudbeck
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Patent number: 6897308Abstract: A process for the preparation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one of the formula IIB: where X may be halo, acyloxy, or sulfonyloxy such as tosyloxy or mesyloxy, an intermediate in the synthesis of the anti-psychotic risperidone. The process comprises hydrogenation of 3-substituted ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in aqueous inorganic acid medium at atmospheric to 60 psi at 0-100° C. in the presence of a metal catalyst and the product is isolated. A process for the preparation of risperidone of the formula I: comprising condensation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one with 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole in water in the presence of an inorganic base at 25-100° C. and the product is isolated.Type: GrantFiled: May 5, 2000Date of Patent: May 24, 2005Assignee: RGP Life Sciences LimitedInventors: Radhakrishnan Tarur Venkatasubramanian, Sathe Dhananjay Govind, Suryavanshi Chandrakant Vasantrao
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Patent number: 6878700Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: March 31, 2000Date of Patent: April 12, 2005Assignee: Abbott LaboratoriesInventors: James Link, Gang Liu, ZhongHua Pei, Tom von Geldern, Martin Winn, Zhili Xin, Steven A. Boyd, Gui-Dong Zhu, Jennifer C. Freeman, Indrani W. Gunawardana, Michael A. Staeger, Hwan-Soo Jae, John K. Lynch, Sheldon Wang
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Patent number: 6875771Abstract: Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.Type: GrantFiled: July 15, 2003Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Shuanghua Hu, Paul M. Scola, Yazhong Huang, Katharine A. Grant-Young
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Patent number: 6864259Abstract: The present invention provides compounds of Formula (I): wherein R1-R6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antibacterial agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: May 29, 2002Date of Patent: March 8, 2005Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Kim Marie Hutchings, Dai Nguyen, Rajeshwar Singh, Howard Daniel Hollis Showalter
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Patent number: 6858613Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 22, 2005Assignee: Pfizer Inc.Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Patent number: 6828326Abstract: The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula wherein A, B, X, Y, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating arthritis, inflammation, cancer and other disorders.Type: GrantFiled: August 5, 2003Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Michael William Wilson
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Publication number: 20040235865Abstract: The imidazo[1,2-a]pyrimidines given by the following formula [I]: 1Type: ApplicationFiled: March 2, 2004Publication date: November 25, 2004Inventor: Hiroshi Ikegami
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Patent number: 6803055Abstract: Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes microparticles that exhibit diffusional release and microparticles that exhibit biodegradation release.Type: GrantFiled: February 6, 2003Date of Patent: October 12, 2004Assignees: Alkermas Controlled Therapeutics Inc. II, Janssen PharmaceuticaInventors: Jean Mesens, Michael E. Rickey, Thomas J. Atkins
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Publication number: 20040176396Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis.Type: ApplicationFiled: November 12, 2003Publication date: September 9, 2004Inventors: Tesfaye Biftu, Richard Beresis, Richard Berger, Steven L Coletti, James B Doherty, Dennis D Feng, Gui-Bai Liang, Dennis M Schmatz, Xiaoxia Qian, David A Claremon, Nigel J Liverton, Charles J McIntyre, Ernest W Kovacs
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Patent number: 6784293Abstract: The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials.Type: GrantFiled: June 25, 2002Date of Patent: August 31, 2004Assignee: The Procter & Gamble CompanyInventors: Shengde Wu, John Michael Janusz
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Patent number: 6762181Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.Type: GrantFiled: September 7, 2001Date of Patent: July 13, 2004Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
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Patent number: 6750341Abstract: The present invention is directed to the novel forms of risperidone, designated Form A, Form B and Form E. Methods for their preparation are also disclosed. The present invention also relates to processes for making risperidone. Pharmaceutical compositions containing the new forms of risperidone and methods of using them are also disclosed.Type: GrantFiled: August 14, 2001Date of Patent: June 15, 2004Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Barnaba Krochmal, Dov Diller, Ben-Zion Dolitzky, Judith Aronhime
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Patent number: 6747032Abstract: Compound of formula (I): wherein: R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen atom, a halogen atom or a group selected from alkyl, alkoxy, polyhaloalkyl, hydroxy, cyano, nitro and amino, or R1 with R2, R2 with R3, or R3 with R4, together with the carbon atoms carrying them, form an optionally substituted benzene ring or an optionally substituted heteroaromatic ring, X represents an oxygen atom or a methylene group, A represents an alkylene chain, represents an optionally substituted, unsaturated, nitrogen-containing heterocycle and R5 represents an alkyl group, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid, a medicinal products containing the same are useful as a double &agr;2/5-HT2c antagonist.Type: GrantFiled: April 18, 2002Date of Patent: June 8, 2004Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Thierry Dubuffet, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Patent number: 6740656Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, R1, R2, R3a, R3b, R4, R5, R6, and n are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: August 2, 2002Date of Patent: May 25, 2004Assignee: Neurocrine Biosciences, Inc.Inventors: Joseph Pontillo, Chen Chen
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Publication number: 20040092533Abstract: A class of imidazo[1,2-&agr;]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.Type: ApplicationFiled: September 19, 2003Publication date: May 13, 2004Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Mark Stuart Chambers, Simon Charles Goodacre, David James Hallett, Philip Jones, Richard Thomas Lewis, Angus Murray MacLeod, Robert James Maxey, Kevin William Moore, Leslie Joseph Street
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Publication number: 20040058938Abstract: The use of substituted imidazoazines of the formula I, 1Type: ApplicationFiled: June 4, 2003Publication date: March 25, 2004Inventors: Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Frank Schieweck, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: RE39197Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: August 29, 2002Date of Patent: July 18, 2006Assignee: Abbott LaboratoriesInventors: James T. Link, Gang Liu, Zhonghua Pei, Tom von Geldern, Martin Winn, Zhili Xin